RU2014153920A - Dihydronaphthyridines and Related Compounds Suitable as Kinase Inhibitors for the Treatment of Proliferative Diseases - Google Patents
Dihydronaphthyridines and Related Compounds Suitable as Kinase Inhibitors for the Treatment of Proliferative Diseases Download PDFInfo
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- RU2014153920A RU2014153920A RU2014153920A RU2014153920A RU2014153920A RU 2014153920 A RU2014153920 A RU 2014153920A RU 2014153920 A RU2014153920 A RU 2014153920A RU 2014153920 A RU2014153920 A RU 2014153920A RU 2014153920 A RU2014153920 A RU 2014153920A
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- Prior art keywords
- oxo
- dihydro
- naphthyridin
- ethyl
- fluorophenyl
- Prior art date
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Abstract
1. Способ лечения заболевания, вызванного киназной активностью c-KIT, ее онкогенных форм или полиморфов, включающий введение соединения формулы Iaили его фармацевтически приемлемой соли,где:A выбран из группы, состоящей из фенила, нафтила и бензотиенила;G1 представляет собой гетероарил, выбранный из группы, состоящей из пирролила, фурила, тиенила, оксазолила, тиазолила, изоксазолила, изотиазолила, имидазолила, пиразолила, оксадиазолила, тиадиазолила, триазолила, тетразолила, пиразинила, пиридазинила, триазинила, пиридинила и пиримидинила;G4 представляет собой гетероциклил, выбранный из группы, состоящей из оксетанила, азетадинила, тетрагидрофуранила, пирролидинила, оксазолинила, оксазолидинила, имидазолонила, пиранила, тетрагидропиранила, диоксалинила, пиперидинила и морфолинила;если A имеет один или более sp2-гибридизованных атомов углерода, которые могут иметь заместители, то каждый соответствующий sp2-гибридизованный атом углерода может быть необязательно замещен заместителем Z3;Z1 выбран из группы, состоящей из -NH(R4) и -NHCOR8;в случае если Z1 содержит алкильный или алкиленовый фрагмент, указанные фрагменты могут быть дополнительно замещены одним или более C1-C6 алкилами;каждый Z2 независимо по отдельности выбран из группы, состоящей из водорода, C1-C6 алкила, C3-C8 карбоциклила, C1-C6 алкокси, гидроксила, гидрокси-C1-C6 алкила, циано, (R3)N- и -(CH)R5;в случае если Z2 содержит алкильный или алкиленовый фрагмент, то указанные фрагменты могут быть дополнительно замещены одним или более C1-C6 алкилами;каждый Z3 независимо по отдельности выбран из группы, состоящей из H, метила, этила, изопропила, C3-C4 карбоциклила, галогена, циано, -(CH)-N(R3)и -(CH)-R5;R1 выбран из группы, состоящей из C1-C4 алкила, разветвленного C3-C5 алкила и C3-C5 карбоци1. A method of treating a disease caused by the kinase activity of c-KIT, its oncogenic forms or polymorphs, comprising administering a compound of formula Ia or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of phenyl, naphthyl and benzothienyl; G1 is heteroaryl selected from the group consisting of pyrrolyl, furyl, thienyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyrazinyl, pyridazinyl, triazinyl, pyridinyl and 4; is heterocyclyl selected from the group consisting of oxetanyl, azetadinyl, tetrahydrofuranyl, pyrrolidinyl, oxazolinyl, oxazolidinyl, imidazolonyl, pyranyl, tetrahydropyranyl, dioxalinyl, piperidinyl and morpholinyl; if A has one or more substituted carbon atoms, sp , then each corresponding sp2-hybridized carbon atom may be optionally substituted with Z3; Z1 is selected from the group consisting of -NH (R4) and -NHCOR8; if Z1 contains an alkyl or alkylene fr an agent, said fragments may be further substituted with one or more C1-C6 alkyls; each Z2 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C3-C8 carbocyclyl, C1-C6 alkoxy, hydroxyl, hydroxy-C1- C6 alkyl, cyano, (R3) N- and - (CH) R5; if Z2 contains an alkyl or alkylene fragment, these fragments may be further substituted with one or more C1-C6 alkyls; each Z3 is independently selected from the group consisting of H, methyl, ethyl, isopropyl, C3-C4 carbocyclyl, halogen, cyano, - (CH) -N (R3) and - (CH) -R5; R1 selected from the group consisting of C1-C4 alkyl, branched C3-C5 alkyl, and C3-C5 carboci
Claims (30)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/US2012/041378 WO2013184119A1 (en) | 2012-06-07 | 2012-06-07 | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2018107578A Division RU2804468C2 (en) | 2018-03-01 | Dihydronaphthyridines and related compounds suitable as kinase inhibitors for the treatment of proliferative diseases |
Publications (2)
Publication Number | Publication Date |
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RU2014153920A true RU2014153920A (en) | 2016-07-27 |
RU2664055C2 RU2664055C2 (en) | 2018-08-14 |
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RU2014153920A RU2664055C2 (en) | 2012-06-07 | 2012-06-07 | Dihydronaphthyridines and related compounds suitable as kinase inhibitors for treatment of proliferative diseases |
Country Status (26)
Country | Link |
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EP (3) | EP3366293B1 (en) |
JP (1) | JP5883195B2 (en) |
KR (1) | KR101652229B1 (en) |
CN (3) | CN110433162A (en) |
AU (1) | AU2012327210B2 (en) |
BR (1) | BR112014030577B1 (en) |
CA (1) | CA2875970C (en) |
CY (1) | CY1123377T1 (en) |
DK (2) | DK2858646T3 (en) |
ES (2) | ES2663605T3 (en) |
FR (1) | FR22C1013I2 (en) |
HK (1) | HK1209345A1 (en) |
HR (1) | HRP20200864T1 (en) |
HU (2) | HUE049958T2 (en) |
IL (1) | IL236110A (en) |
LT (2) | LT3366293T (en) |
MX (2) | MX2020005712A (en) |
NO (1) | NO2022010I1 (en) |
PH (2) | PH12014502757A1 (en) |
PL (1) | PL3366293T3 (en) |
PT (2) | PT2858646T (en) |
RS (1) | RS60406B1 (en) |
RU (1) | RU2664055C2 (en) |
SG (1) | SG11201408133TA (en) |
SI (1) | SI3366293T1 (en) |
WO (1) | WO2013184119A1 (en) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
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US8461179B1 (en) | 2012-06-07 | 2013-06-11 | Deciphera Pharmaceuticals, Llc | Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
CN111793068A (en) | 2013-03-15 | 2020-10-20 | 西建卡尔有限责任公司 | Heteroaryl compounds and uses thereof |
EP3943087A1 (en) | 2013-03-15 | 2022-01-26 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
RS62626B1 (en) | 2016-01-11 | 2021-12-31 | Merck Patent Gmbh | Quinolin-2-one derivatives |
CN111328283A (en) * | 2017-05-30 | 2020-06-23 | 德西费拉制药有限责任公司 | Use of 1- [ 4-bromo-5- [ 1-ethyl-7- (methylamino) -2-oxo-1, 2-dihydro-1, 6-naphthyridin-3-yl ] -2-fluorophenyl ] -3-phenylurea and analogs for the treatment of cancer associated with genetic abnormalities in platelet-derived growth factor receptor α |
WO2019056990A1 (en) * | 2017-09-20 | 2019-03-28 | 浙江海正药业股份有限公司 | 1,2-dihydro-1,6-naphthyridine derivative, preparation method therefor, and application thereof in medicine |
CA3089566A1 (en) * | 2018-01-31 | 2019-08-08 | Deciphera Pharmaceuticals, Llc | Combination therapy for the treatment of gastrointestinal stromal tumors |
WO2020185812A1 (en) * | 2019-03-11 | 2020-09-17 | Teva Pharmaceuticals International Gmbh | Solid state forms of ripretinib |
CN114072148A (en) | 2019-05-03 | 2022-02-18 | 金耐特生物制药公司 | Inhibitors of RAF kinase |
MX2022001863A (en) | 2019-08-12 | 2022-05-30 | Deciphera Pharmaceuticals Llc | Ripretinib for treating gastrointestinal stromal tumors. |
WO2021030405A1 (en) | 2019-08-12 | 2021-02-18 | Deciphera Pharmaceuticals, Llc | Ripretinib for treating gastrointestinal stromal tumors |
EP4048259A4 (en) | 2019-10-24 | 2023-08-02 | Kinnate Biopharma Inc. | Inhibitors of raf kinases |
BR112022013169A2 (en) | 2019-12-30 | 2022-09-13 | Deciphera Pharmaceuticals Llc | COMPOSITIONS OF 1-(4-BROMO-5-(1-ETHYL-7-(METHYLAMINO)-2-OXO-1,2-DIHYDRO-1,6-NAFTIRIDIN-3-YL)-2-FLUOROFEYL)-3- PHENYLUREA |
RS65058B1 (en) | 2019-12-30 | 2024-02-29 | Deciphera Pharmaceuticals Llc | Amorphous kinase inhibitor formulations and methods of use thereof |
KR102535840B1 (en) * | 2020-07-31 | 2023-05-23 | (주)파로스아이바이오 | Use of 2,3,5-Substituted Thiophene Compound for Prevention, Improvement or Treatment of Gastrointestinal Stromal Tumor |
US11407737B2 (en) | 2020-09-18 | 2022-08-09 | Kinnate Biopharma Inc. | Inhibitors of RAF kinases |
WO2022081469A1 (en) | 2020-10-12 | 2022-04-21 | Kinnate Biopharma Inc. | Inhibitors of raf kinases |
CN112625038A (en) * | 2020-12-31 | 2021-04-09 | 武汉九州钰民医药科技有限公司 | Method for preparing Ripoctinib |
WO2022162690A1 (en) * | 2021-01-28 | 2022-08-04 | Dr. Reddy's Laboratories Limited | Process for the preparation of ripretinib and solid state forms thereof |
CA3216104A1 (en) | 2021-04-23 | 2022-10-27 | Aleksandra Franovic | Treatment of cancer with a raf inhibitor |
WO2023122322A1 (en) * | 2021-12-24 | 2023-06-29 | Teva Pharmaceuticals International Gmbh | Improved processes for the preparation of ripretinib |
CN114213411B (en) * | 2022-01-24 | 2023-06-30 | 成都伊诺达博医药科技有限公司 | Synthesis method of rapatinib |
US11814384B2 (en) | 2022-02-03 | 2023-11-14 | Kinnate Biopharma Inc. | Inhibtors of Raf kinases |
US11779572B1 (en) | 2022-09-02 | 2023-10-10 | Deciphera Pharmaceuticals, Llc | Methods of treating gastrointestinal stromal tumors |
Family Cites Families (6)
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BRPI0415210A (en) * | 2003-10-08 | 2006-12-05 | Irm Llc | compounds and compositions as protein kinase inhibitors |
DE102006030524A1 (en) * | 2006-07-01 | 2008-01-03 | Koch Transporttechnik Gmbh | Method for removing loose coal from corrugated surfaces of long narrow coal cake comprises moving the loose coal from peaks into troughs and holding on the coal cake |
CN101553232A (en) * | 2006-09-14 | 2009-10-07 | 迪赛孚尔制药有限公司 | Kinase inhibitors useful for the treatment of proliferative diseases |
US8188113B2 (en) * | 2006-09-14 | 2012-05-29 | Deciphera Pharmaceuticals, Inc. | Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases |
CA2667010A1 (en) * | 2006-10-20 | 2008-05-02 | Irm Llc | Compositions and methods for modulating c-kit and pdgfr receptors |
BRPI0908849A2 (en) * | 2008-02-22 | 2015-08-25 | Irm Llc | Compound and compositions as c-kit and pdgfr kinase inhibitors |
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